链霉素特异性抑制细胞和大肠杆菌提取物中的蛋白质合成。 E 被壮观霉素 (50 μg/mL) 快速且可逆地抑制。大肠杆菌生长和氨基酸掺入的迅速阻断[1]。内源性信使 RNA 或 MS-2 噬菌体 RNA 刺激的肽合成会被壮观霉素（1 μg/mL 或 3 μM）抑制，在大肠杆菌提取物中最大抑制率为 70-80% [1]。 Spectinomycin 抑制延伸因子 G 与核糖体的结合，防止肽基 tRNA 从 A 位点易位至 P 位点 [2]。 16S rRNA 中的试剂 G1064 和 01192 特别与壮观霉素相互作用，并可能使其失去活性 [2]。由于其对 pH 变化和 Mg2+ 浓度的依赖性，spezinominosinomycin 显示出剪接抑制作用，这可能表明与内含子 RNA 存在静电相互作用 [3]。

已证明，在健康雏鸡中，百替霉素（20 mg/kg；肌肉注射；20-100 mg/kg；9 天）是安全的[4]。大部分大奇霉素（10 mg/kg；静脉注射；单剂量）通过肾脏排泄，其中约 55% 不发生改变地通过尿液排出[5]。大鼠大观霉素药代动力学 [5] 规格 C0 μg/mL AUC0-∞ (μg^h/mL) Vd (升/千克) CL (升/小时/kg) MRT (小时) T1/2α (小时) T1 /β ( h）T1 /2γ（小时）Fe clenal（kg / h / h）inratio分析，未分隔1.00 44.3 16.8 0.756 0.756 0.757 / / / / / 0.553 0.359 0.359三段模型37.8 15.7 0.7471.11.11.11 / 0.2377 0.757 0.7554 0.754 0.754 19.54 19.54 19.54 19.54 19.54 19.54 19.54 19.55 ///////////////////////////////////////////////////////////////////////////////////////////////////////////////////////// /

Animal/Disease Models: Arbor Acres plus broiler chicken (15 days old) [4]
Doses: 20 mg/kg, 60 mg/kg, 100 mg/kg
Route of Administration: intramuscularinjection (chest muscle); 9-day
Experimental Results: Complete blood count, biochemical parameters, histopathology, clinical signs, weight gain and feed conversion ratio (FCR) demonstrated biosafety of 20 mg/kg. Produces mild toxicity at 60 mg/kg.

Absorption, Distribution and Excretion
Rapid and almost complete absorption after intramuscular injection. Biological Half-Life 1 to 3 hours in patients with normal renal function, and 10 to 30 hours in patients with impaired renal function and creatinine clearance < 20 mL/min.

Protein Binding

Not significant

[1]. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.

[2]. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31.

[3]. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9.

[4]. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209.

[5]. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.

Spectinomycin is a pyranobenzodioxin antibiotic effective against Gram-negative bacteria. Its dihydrochloride pentahydrate is used to treat gonorrhea. It is produced by Streptomyces spectabilis. Spectinomycin has antibacterial activity and is both a bacterial metabolite and an antibacterial drug. It is a cyclic hemiacetal, cyclic acetal, cyclic ketone, secondary amino compound, pyranobenzodioxin, and secondary alcohol. It is the conjugate base of spectinomycin (2+) and spectinomycin (1+).
An antibiotic produced by Streptomyces spectabilis. It is effective against Gram-negative bacteria and used to treat gonorrhea.
Spectinomycin has been reported in Streptomyces, Streptomyces reticulata, and other microorganisms with relevant data.
Spectinomycin hydrochloride is the hydrochloride form of spectinomycin, an aminocyclic alcohol antibiotic derived from Streptomyces spectabilis with antibacterial activity. Spectinomycin hydrochloride binds to the 30S ribosomal subunit of bacteria, thereby inhibiting peptide chain elongation and protein synthesis, ultimately leading to bacterial death.
Spectinomycin is an aminocyclic alcohol aminoglycoside antibiotic derived from Streptomyces spectabilis, possessing antibacterial activity. Spectinomycin binds to the 30S ribosomal subunit of bacteria. Therefore, the drug interferes with the initiation of protein synthesis and normal protein elongation. This ultimately leads to bacterial cell death.
An antibiotic produced by Streptomyces spectabilis. It is effective against Gram-negative bacteria and is used to treat gonorrhea.

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Indications
For the treatment of acute gonococcal urethritis and proctitis in men, and acute gonococcal cervicitis and proctitis in women, caused by susceptible strains of Neisseria gonorrhoeae.

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Mechanism of Action
Spectinomycin is an inhibitor of intracellular bacterial protein synthesis; its site of action is the 30S ribosomal subunit. It has bactericidal activity.

332.35

332.158

1695-77-8

Spectinomycin dihydrochloride;21736-83-4;Spectinomycin dihydrochloride pentahydrate;22189-32-8

15541

Typically exists as solid at room temperature

1.43 g/cm3

583.1ºC at 760 mmHg

185ºC

5.05E-16mmHg at 25°C

-3.1

130

5

9

2

23

478

9

C[C@@H]1CC(=O)[C@]2([C@@H](O1)O[C@@H]3[C@H]([C@@H]([C@@H]([C@@H]([C@H]3O2)NC)O)NC)O)O

UNFWWIHTNXNPBV-WXKVUWSESA-N

InChI=1S/C14H24N2O7/c1-5-4-6(17)14(20)13(21-5)22-12-10(19)7(15-2)9(18)8(16-3)11(12)23-14/h5,7-13,15-16,18-20H,4H2,1-3H3/t5-,7-,8+,9+,10+,11-,12-,13+,14+/m1/s1

(1R,3S,5R,8R,10R,11S,12S,13R,14S)-8,12,14-trihydroxy-5-methyl-11,13-bis(methylamino)-2,4,9-trioxatricyclo[8.4.0.03,8]tetradecan-7-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。